1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. PDI
  3. KSC-34

KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family. KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

KSC-34 Chemical Structure

KSC-34 Chemical Structure

CAS No. : 2226201-97-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 500 In-stock
25 mg USD 1050 In-stock
50 mg USD 1650 In-stock
100 mg USD 2550 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family[1]. KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IC50: 3.5 μM (a active site of PDIA1), 104.5 μM (a′ active site of PDIA1)[1]

In Vitro

KSC-34 is selective for PDIA1 over other members of the PDI family, and other cellular cysteine-containing proteins. KSC-34 contains a (4-phenylbutyl)methylamine diversity element for optimized binding to the active site of the a domain of PDIA1 with a chloroacetamide electrophile for covalent modification of C53 on PDIA1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

429.95

Formula

C21H28ClN7O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCNC1=NC(N(C)CCCCC2=CC=CC=C2)=NC(NCC#C)=N1)CCl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (232.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3259 mL 11.6293 mL 23.2585 mL
5 mM 0.4652 mL 2.3259 mL 4.6517 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3259 mL 11.6293 mL 23.2585 mL 58.1463 mL
5 mM 0.4652 mL 2.3259 mL 4.6517 mL 11.6293 mL
10 mM 0.2326 mL 1.1629 mL 2.3259 mL 5.8146 mL
15 mM 0.1551 mL 0.7753 mL 1.5506 mL 3.8764 mL
20 mM 0.1163 mL 0.5815 mL 1.1629 mL 2.9073 mL
25 mM 0.0930 mL 0.4652 mL 0.9303 mL 2.3259 mL
30 mM 0.0775 mL 0.3876 mL 0.7753 mL 1.9382 mL
40 mM 0.0581 mL 0.2907 mL 0.5815 mL 1.4537 mL
50 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1629 mL
60 mM 0.0388 mL 0.1938 mL 0.3876 mL 0.9691 mL
80 mM 0.0291 mL 0.1454 mL 0.2907 mL 0.7268 mL
100 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5815 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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KSC-34
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HY-117570
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